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enoxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 1013 | 74011-58-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.60 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 45 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 62.44 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 87 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 2 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.80 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.10 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.691 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.524 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 4.842 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.104 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 81.850 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 85.250 | % | High | 1 |
| herg | hERG pIC50 | 4.663 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.140 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.451 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 79.250 | % | High | 1 |
| kinase-safety-class | ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PRKDC | 6 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK7,PIK3CB,PIK3CD,PRKDC,SIK2,STK33,SYK,TEK,TTK | 19 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 10.520 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.688 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 85.340 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 12.735 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 85.570 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.799 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.090 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 66.250 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 870.964 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 31, 1991 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01MA04 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| MeSH PA | D065607 | Cytochrome P-450 Enzyme Inhibitors |
| MeSH PA | D065609 | Cytochrome P-450 CYP1A2 Inhibitors |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:59517 | DNA synthesis inhibitor |
Related Drugs by ATC class:
J01MA Fluoroquinolones 22 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Gonorrhea | indication | 15628003 | DOID:7551 |
| Acute gonococcal cervicitis | indication | 20943002 | DOID:10615 |
| Acute gonococcal urethritis | indication | 29864006 | |
| Gonorrhea of rectum | indication | 42746002 | |
| Urinary tract infectious disease | indication | 68566005 | |
| Gonorrhea of pharynx | indication | 74372003 | |
| Chancroid | off-label use | 266143009 | DOID:13778 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.14 | acidic |
| pKa2 | 8.63 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| V-type proton ATPase subunit B, brain isoform | Enzyme | IC50 | 5 | CHEMBL | |||||
| RISC-loading complex subunit TARBP2 | Cytosolic other | Kd | 7.03 | CHEMBL | |||||
| Topoisomerase IV | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| DNA gyrase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| DNA gyrase subunit A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4020144 | VUID |
| N0000148115 | NUI |
| D00310 | KEGG_DRUG |
| 4020144 | VANDF |
| C0014310 | UMLSCUI |
| CHEBI:157175 | CHEBI |
| CHEMBL826 | ChEMBL_ID |
| DB00467 | DRUGBANK_ID |
| D015365 | MESH_DESCRIPTOR_UI |
| 3229 | PUBCHEM_CID |
| 8882 | IUPHAR_LIGAND_ID |
| 5351 | INN_ID |
| 325OGW249P | UNII |
| 3925 | RXNORM |
| 4658 | MMSL |
| d00099 | MMSL |
| 003660 | NDDF |
| 387550004 | SNOMEDCT_US |
| 96084004 | SNOMEDCT_US |
Pharmaceutical products:
None